Abstract: The invention provides a peptide triazole conjugate and derivatives thereof, and methods of its use. The invention also provides an antibody to the peptide triazole conjugate. The invention further provides a method of identifying an HIV-1 entry inhibitor candidate.

Abstract: The present invention relates to a method for the purification of cyclopeptides of general formula (3) by means of a silicate.

Abstract: Provided is niacin-peptide which has skin whitening activity. The peptide of the present invention has skin whitening activity by inhibiting melanogenesis, that is, by inhibiting the expression of a gene related to melanogenesis (for example, TRP-1, TRP2, or MIFT). The peptide of the present invention has high stability and skin permeability. Also provided is a cosmetic composition for skin whitening which contains the niacin-peptide.

Abstract: Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs: R1-A1-A2-A3-A4-A5-R2??(I) wherein: A1 is Aib, Apc or Inp; A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A5 is Apc, Dab, Dap, Lys, Orn, or deleted; R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R2 is OH or NH2; and pharmaceutical compositions and methods of use thereof.

Abstract: A method for screening a drug for cytochrome P450 (CYP) induction is provided and can include incubating the drug with a microsome-containing biological sample and then quantitating at least one cytochrome P450 isoform. The isoforms can be selected from 2B6, 3A4, 1A2, and 3A5 isoforms. In some embodiments, the method uses liquid chromatography tandem mass spectrometry (LC-MSMS). A quantitated value can be compared to a threshold value and the drug can be determined to exhibit an acceptable CYP induction potential when the quantitated value does not exceed the threshold value. Isolated peptides are also provided.

Abstract: Compositions, methods of making, and methods of using, xenoantigen-displaying anticancer vaccines are described. In another broad aspect, there is provided herein a method of synthesizing an alkynefunctionalized composition of claim 1, comprising: deprotecting an ester comprising a Fmoc moiety to form a free acid; coupling the free acid of step (a) with an amine; and, removing the Fmoc moiety, and coupling the remaining moiety with palmitic acid to yield an alkyne-functionalized composition.

Abstract: The invention relates to novel interfering peptides having peptide sequence S with between 7 and 12 amino acids, originating from the peptide sequence of an antigenic protein of a micro-organism M, the sequence S being aligned with a peptide sequence S? with between 7 and 12 amino acids originating from the peptide sequence of a target protein of a micro-organism M? that is different from the micro-organism M, provided that: sequences S and S? have at least 50% identity over their length of 7 to 12 amino acids and at least 4 identical or analogous contiguous amino acids; and their length is identical or they have 1 or 2 different amino acids distributed at one and/or the other end of the sequences. The invention also relates to a method for the in vitro immunoassay-based detection of the presence of a micro-organism M? or M in a biological sample.

Abstract: Cyclohexapeptides of formula (I): as defined herein. The cyclohexapeptides are non-selective functional analogs of somatostatin.

Abstract: The invention provides novel immunological adjuvants and methods for identification of such adjuvants. The invention further provides methods and compositions for eliciting an immune response to an immunogen using the novel adjuvants. The adjuvants can be employed with any suitable immunogen, including proteins, peptides, lipids, and carbohydrates. The immunogen can be derived from a virus, a cancer, or a diseased cell. The elicited immune response can be cellular, humoral, or both.

Abstract: The present invention relates to disorder-specific epitopes recognized by myeloperoxidase-anti-neutrophil cytoplasmic autoantibodies and the use of polypeptides comprising the epitopes in methods of diagnosing and monitoring autoimmune disorders associated with the autoantibodies.

Abstract: The subject matter of the present invention is peptide C?-amides which are precursors of peptide C?-thioesters, characterized in that they comprise the radical of general formula (I) in which X, R1, R2, R3, R4, R5, R6, R7, R8, R9, n and A are as defined in Claim 1. The subject matter of the present invention is also the use of these peptide C?-amides for obtaining peptide C?-thioesters. The subject matter of the present invention is also the use of these peptide C?-amides for obtaining peptides or proteins, in particular of therapeutic interest, by direct use as a crypto-thioester partner in NCL reactions.

Abstract: In certain embodiments compositions are provided that comprise a pentapeptide comprising the formula: C1-X2-X3-X4-C5 where C1 and C5 are independently selected cysteines or cysteine analogues, or other amino acids with sidechains suitable for cyclization, where the cysteines or cysteine analogs are attached to each other by a linkage that does not comprise X2, X3, and X4; where X2, X3, and X4 are independently selected amino acids; and the peptide, when administered to a cell alters APP signaling and/or switches APP processing from aberrant to normal. The compositions mitigate amyloid plaque formation.

Abstract: The invention provides an isolated peptide comprising a lysine 2-hydroxyisobutyrylation site, a lysine 2-hydroxyisobutyrylation specific affinity reagent that specifically binds to the peptide, and a method for detecting protein lysine 2-hydroxyisobutyrylation in a sample using the reagent.

Abstract: The present disclosure provides conjugates, systems, devices, and methods for detecting cellular redox state. In one aspect, for example, a conjugate for detecting cellular redox state can include a first segment including a cell penetrating peptide conjugated to a first detection molecule, and a second segment including a cargo peptide conjugated to a second detection molecule, wherein the first segment and the second segment are coupled together by a redox-sensitive linkage, and wherein the first detection molecule and the second detection molecule have properties that allow linked proximity detection. In one specific example, the first detection molecule and the second detection molecule include fluorophore/quencher pair.

Abstract: A peptide of general formula (I): R1-(AA)nX1-X2-Arg-Arg-Gly-X3-X4-(AA)p-R2, and cosmetic and pharmaceutical compositions are disclosed that include at least one peptide of general formula (I), in a physiologically suitable medium. Also disclosed are methods for activating human transglutaminase to reinforce the skin barrier function and to stimulate epidermal regeneration and differentiation or for cosmetic treatment to treat signs of skin ageing, which include administering a composition containing the peptide of general formula (I) as an active ingredient.

Abstract: Melanocortin receptor-specific linear peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification, compositions and formulations including peptides of the foregoing formula or salts thereof, and pharmaceutical compositions for preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.

Abstract: The present invention relates to the use of which are attached or anchored phospholipid biolayers further modified by CRLF-2 and CD 19 binding peptides which may be used for delivering pharmaceutical cargos, to cells expressing CRLF-2 and CD 19, thereby treating cancer, in particular, acute lymphoblastic leukemia (ALL), including (B-precursor acute lymphoblastic leukemia (B-ALL). Novel CRLF-2 binding peptides and CLRF-2 and CD19-binding viral-like particles (VLPs) useful in the treatment of cancer, including ALL are also provided.

Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula I: The peptoids demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present cyclic and linear peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.

Abstract: Isolated polypeptides that are endogenously expressed from nucleotide repeat expansions are disclosed. In some cases, the polypeptides include polypeptide repeats. In some cases, the polypeptide repeats include at least five contiguous repeats of a single amino acid. In other cases, the repeats include at least six contiguous amino acids of a tetra- or penta-amino acid repeat block.

Abstract: The invention relates to a peptide comprising the following amino acid sequence Thr-Phe-Leu-Lys or Thr-Phe-Leu-Lys-Cys, useful as a CCR2 non competitive antagonist peptide.

Abstract: The invention provides a peptide triazole conjugate and derivatives thereof, and methods of its use.

Abstract: The present invention relates to prodrugs of vascular disrupting agents comprising a vascular disrupting agent (VDA) associated with a matrix metalloproteinase (MMP) proteolytic cleavage site and to the use of such prodrugs in the targeted treatment of cancer.

Abstract: A system for targeted delivery of agents (e.g., molecular probes, diagnostic agents, therapeutic agents, imaging agents, research or analytical compounds, enzymes, peptides, proteins, lipids, lipoproteins, sugars, hormones, vitamins, nucleic acids, viruses, bacteria, and/or cells) including use of a composition containing the agent and a targeting moiety, specific for a determinant at the target location. An exemplary composition of the system includes a targeting moiety of one of peptides ?3, 2?3, 3?3, A1, B7, B8, B9, B1O, and D6, specific for targeting ICAM-I. The system enables effective, versatile, and safe targeting and transport of agents. The system is useful in research applications, as well as in the context of translational science and clinical interventions.

Abstract: PAR4 agonist peptides are disclosed. These peptides are useful for developing robust PAR4 receptor assays.

Abstract: The present invention provides a pharmaceutical composition for the sustained release of C-peptide. The composition is in the form of a gel containing C-peptide. The gel formation is achieved by the adjustment of pH of the composition and/or by addition of divalent metal ions. The composition does not include any other gel-forming agents. Methods for producing the composition, medical uses of the composition and products containing two or more gel compositions as a combined preparation are also encompassed.

Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.

Abstract: The disclosure provides aromatic-cationic peptide compositions and methods of preventing or treating disease using the same. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof.

Abstract: The invention relates to common allergen proteins and peptides, subsequences, portions, homologues, variants and derivatives thereof, and methods and uses of common allergen proteins and peptides. Methods include, for example, modulating an immune response; protecting a subject against or treating a subject for an allergic response, allergic disorder or allergic disease; and inducing immunological tolerance to the allergen in a subject.

Abstract: The present invention relates to a process for the production of bivalirudin, a 20-mer peptide of formula H-(D)-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH (SEQ ID NO: 1).

Abstract: The present invention provides methods of specifically targeting compounds to cells overexpressing matrix metalloproteinases, plasminogen activators, or plasminogen activator receptors, by administering a compound and a mutant protective antigen protein comprising a matrix metalloproteinase or a plasminogen activator-recognized cleavage site in place of the native protective antigen furin-recognized cleavage site, wherein the mutant protective antigen is cleaved by a matrix metalloproteinase or a plasminogen activator overexpressed by the cell, thereby translocating into the cell a compound comprising a lethal factor polypeptide comprising a protective antigen binding site.

Abstract: The present invention relates to expression vectors and methods for enhancing soluble expression and secretion of an insoluble heterologous protein, particularly a bulky folded active heterologous protein which has one or more transmembrane-like domains or intramolecular disulfide bonds by linking a leader peptide with acidic or basic pl and high hydrophilicity thereto; by substituting one or more amino acids within N-terminal of the heterologous protein with ones having acidic or neutral pl and high hydrophilicity; or reducing elevating ?GRNA value of a polynucleotide encoding the leader peptide having basic pl value and high hydrophilicity. The expression vector and the method may be used to produce of heterologous protein and to transduce of therapeutic proteins in a patient by preventing formation of insoluble inclusion body and by enhancing secretional efficiency of the heterologous protein into the periplasm or outside cell.

Abstract: The present invention relates to a method for the purification of Micafungin.

Abstract: The present invention relates to an improved process for the preparation of Micafungin.

Abstract: The invention is directed to peptides. Specifically, the invention is directed to peptides which bind skin and do not bind hair. Alternatively, the invention is drawn to peptides which bind hair and do not bind skin.

Abstract: The invention relates to a peptide compound and its pharmaceutical composition for inhibiting platelet aggregation and preventing/treating thrombogenic diseases. The invention develops pentapeptides and hexapeptides derived from snake venom C-type lectin-like proteins (CLPs) fragments, which can inhibit platelet aggregation and have antithrombotic activity without hemorrhagic tendency. Accordingly, they can be used as potential agents for the prevention and therapy of thrombogenic diseases.

Abstract: Peptides are provided that comprise less than 24 amino acids. The peptides have an amino acid sequence selected from the group consisting of: (a) an amino acid sequence having from 4 to 6 contiguous amino acids of a reference sequence PEPTIDE 1; (b) an amino acid sequence substantially identical to the sequence defined in (a); and (c) a variant of the amino acid sequence defined in (a). Also provided is a non-myristoylated MANS peptide. Various methods of using the peptides are also provided.

Abstract: The present invention concerns methods and compositions that employ peptides that target dorsal root ganglion (DRG) neurons. In particular, the peptides are used to target therapeutic agents, such as proteins, liposomes, or viral particles comprising therapeutic polynucleotides, to one or more peripheral neuropathies or neuropathic pain, for example. In particular cases, the peripheral neuropathies or neuropathic pain is caused directly or indirectly by DRG neuronopathy.

Abstract: The present invention describes peptides comprising phycocyanobilin (PCB), as well as the medical use of said peptides and that of PCB, due to the neuroprotector and/or neuroregenerative effects identified for them. Furthermore, pharmaceutical combinations of said peptides and of PCB with proteins or other peptides with synergic effect justify their use for ischemic or neurodegenerative CNS disease treatment.

Abstract: This application describes a family of compounds acting as ?-arrestin effectors. Such compounds may provide significant therapeutic benefit in the treatment of chronic and acute cardiovascular diseases.

Abstract: Systems and reagents for identification, characterization and/or targeting of particular tissue or cell markers are disclosed. Methods and compositions for in vivo and in vitro targeting of particular targets are also disclosed. Peptides are employed for targeted delivery of therapeutic or imaging agents.

Abstract: The invention provides a method for treating a medical condition, disease, or disorder mediated by a misfolded form of superoxide dismutase (SOD) in a subject in need of treatment. The method optionally comprises administering to the subject a composition comprising a pharmaceutically acceptable vehicle and an agent selected from (1) an exogenous antibody or fragment thereof that binds selectively to the misfolded form of SOD, and/or (2) an immunogen that elicits production of an endogenous antibody that binds selectively to the misfolded form of SOD, and/or (3) a nucleic acid sequence encoding (1) or (2). In certain embodiments, the invention provides methods of treating diseases such as Alzheimer's Disease, Parkinson's Disease or amyotrophic lateral sclerosis using amyotrophic disease-specific epitopes, and compositions including these epitopes. The invention also provides antibodies that bind to monomeric or misfolded SOD1, and not on the molecular surface of native homodimeric SOD1.

Abstract: A PEG-oligopeptide-irinotecan conjugate has the general formula (I) (shown below) and a pharmaceutical composition containing the conjugate are disclosed. In the conjugate, PEG represents polyethylene glycol with a molecular weight of 300-60,000 Daltons; (AA)i represents an oligopeptide, AA represents the same or different amino acids in the oligopeptide; i is an integer of 2-12 representing the number of amino acids in the oligopeptide; j is an integer of 2-12 representing the number of irinotecan connected with the oligopeptide. In the conjugate, each terminal group of PEG can link with multiple irinotecans through oligopeptides, thereby greatly increasing the drug-loading capacity. Modification of the hydrophilic polymer can provide protection for the irinotecan, thereby improving drug absorption, prolonging the action time, enhancing the efficacy, reducing the dose and avoiding the toxic and side-effects.

Abstract: Disclosed herein are methods for large-scale, high-throughput identification of protein-protein interactions and the topologies thereof under physiologically relevant conditions. In one aspect, the disclosure provides methods for identifying one or a plurality of interacting peptides within a biological system comprising obtaining a population of proteins cross-linked with a cleavable protein interaction reporter (PIR) cross-linker, cleaving the PIR crosslinker to produce released peptides and cleaved reporter ions, and analyzing the population of released peptides to identify interacting peptides. Also disclosed are methods for identifying candidate drug compounds, as well as methods of data processing and visualization of protein-protein interactions.

Abstract: The development of a series of fluorescent materials including heterocycle-functionalized luminogens with aggregation-induced/enhanced emission (AIE/AEE), long wavelength emission, and high solid state fluorescence quantum efficiency is contemplated. The described fluorescent materials are promising candidates in selective luminescence-based chemosensor for Hg2+ or ATP, fluorescent staining for mitochondria in living cells with high photostability, stimuli-responsive luminescent materials, and materials for optical waveguides. In addition, these heterocycle-functionalized luminogens are particularly useful as fluorescent labels for biopolymers such as peptides, antibodies, or nucleic acids, making them useful as AIE-active biocompatible probes for clinical cancer imaging and diagnostics.

Abstract: Synthetic peptides and peptide copolymers for amelioration of autoimmune neurological syndrome, inflammatory and/or demyelinating conditions such as encephalomyletis are provided herein. The synthetic peptides and peptide copolymers as disclosed are obtained by substitution of at least one alpha amino acid by beta amino acid and/or ?3-homo amino acid.

Abstract: N-acylpeptide derivatives are described. Compositions comprising N-acylpeptide derivatives are therapeutically effective for topical or systemic administration to alleviate or improve conditions, disorders, diseases, symptoms or syndromes associated with tumors or cancers, immune, nervous, vascular, musculoskeletal, cutaneous system, or other tissues or systems in a subject.

Abstract: Provided is a method of treating type 2 diabetes in a subject, comprising administering a polypeptide comprising thymosin, or an active fragment or variant thereof, preferably comprising or consisting of the peptide LKKTETQ (SEQ ID NO: 1).

Abstract: A selective targeting method is disclosed comprising contacting a library of ligands, particularly a peptide library, with an anti-target to allow the ligands to bind to the anti-target; separating the non-binding ligands from the anti-target bound ligands, contacting the non-binding anti-target ligands with a target allowing the unbound ligands to bind with the target to form a target-bound ligand complex; separating the target-bound ligand complex from ligands which do not bind to the target, and identifying the target-bound ligands on the target-bound ligand complex wherein the target-bound ligands have a KD in the range of about 10?7 to 10?10 M. Additionally claimed are the ligands identified according to the method.

Abstract: Provided herein are antagonists or binding agents of an abnormal vasopressin receptor V2 (e.g., AbnV2), such as antibodies and antigen-binding portions thereof specific for the receptor, for identifying and targeting cancer cells expressing such abnormal vasopressin receptor V2. Additionally provided are methods of using said antagonists or binding agents, for example, to image cancer cells or in biological samples, or diagnose cancers, both in vivo and in vitro. The antagonists or binding agents may also be used for treating patients suffering from a cancer expressing the abnormal vasopressin receptor V2, such as small cell lung cancer (SCLC), breast cancer, or ovarian cancer.

Abstract: Peptide helices stabilized by backbone cyclization which are capable of inhibiting dimerization of the Chemokine (C-C motif) receptor 2 (CCR2), as well as pharmaceutical compositions including such backbone cyclized peptide helices. Use of pharmaceutical compositions and peptide helices in treatment of Multiple Sclerosis (MS) and other diseases associated with CCR2 activation.